iCDK9

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

iCDK9 (i-CDK9) 是一种有效的、高选择性的 CDK9 抑制剂（IC50<0.4 nM，CDK9-CycT1 激酶），对 CDK1-CycB、CDK2-CycA、CDK4-CycD1、CDK7-CycH-MAT1 表现出 >600 倍的选择性和CDK8-CycC。

iCDK9 (i-CDK9) is a potent, highly selective CDK9 inhibitor (IC50<0.4 nM, CDK9-CycT1 kinase), exhibits >600-fold selectivity toward CDK1-CycB, CDK2-CycA, CDK4-CycD1, CDK7-CycH-MAT1 and CDK8-CycC; potently suppresses CDK9 phosphorylation of substrates and causes genome-wide Pol II pausing; efficiently suppresses P-TEFb's phosphorylation of the Pol II CTD and the DSIF subunit SPT5 and causes widespread Pol II pausing at gene promoters, enhances the MYC mRNA production but not protein stability.

CDK9-IN-2 (200 nM) reduces the expression of MEPCE indicating that MEPCE is a pharmacodynamic (PD) marker for any CDK9 inhibitor. The expression of MCL1 protein is reduced 2 hours after treatment and is further reduced after 16 hour exposure to CDK9-IN-2 (500 nM).

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i-CDK9

Angiogenesis

CDK

CDK

Infection

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1263369-28-3

425.936

C23H25ClFN5

>98% (HPLC)

DMSO : 50 mg/mL 117.39 mM

N[C@@H]1CC[C@H](NC2=NC=C(Cl)C(C3=NC(NCC4=CC(F)=CC=C4)=CC=C3)=C2)CC1

N2'-((1r,4r)-4-aminocyclohexyl)-5'-chloro-N6-(3-fluorobenzyl)-[2,4'-bipyridine]-2',6-diamine

(-20℃)

With Ice Pack

≥ 2 years